Oxidative stress is believed to be one of the key reasons for the development of different eye pathologies.
Mitochondria-addressed antioxidants that can be reduced and oxidized by the enzymes of the electron transport chain of mitochondria are one of the most effective antioxidants (see Skualchev V. P. (2005), IUBMB Life. 57:305-10; Skulachev V. P. (2007) Biochemistry (Mosc.) 72:1385-96; Antonenko Yu. N. et al. (2008) Biochemistry (Mosc.)73:1273-87).
However, said mitochondrial antioxidants have some peculiarities that complicate their use in practice. One of the main peculiarity is the observation that the antioxidant efficiency of a compound depends on its dose and final concentration in mitochondria) in non-obvious way. At certain concentrations these substances can act as one of the most powerful prooxidants that can make mitochondria to produce a significant amount of reactive oxygen species (Antonenko Yu N. et al. (2008) Biochemistry (Mosc.)73:1273-87; Doughan A. K. and Dikalov S. I. (2007) Antioxid Redox Signal. 9:1825-36).
A principle possibility of treating eye diseases with the mitochondria-addressed antioxidant SkQ1 was shown in application WO2008048134, and in more detail in a paper by Neroev et al., (2008) Biochemistry (Mosc.)73:1317-28. These sources report data on the treatment of some eye diseases with the aid of aqueous solutions of SkQ1. However, no ophthalmic pharmaceutical composition comprising mitochondria-addressed is disclosed at the moment. The unusual physicochemical properties of mitochondria-addressed antioxidants make such composition non-obvious. For example, some substances routinely used as part of numerous preparations,—eye drops, accelerate degradation of SkQ1. The ability of SkQ1 to be irreversibly absorbed at the surface of tubes (vials) containing eye drops was also detected. This leads to drastic and uncontrolled change in the concentration of active ingredients in a pharmaceutical composition that, for said reasons, can fundamentally alter the effectiveness of the composition (up to obtaining the results which are completely the opposite of desirable).